L-氨酸玻利乙醇Flurbiprofenate:一种双功能的离子载体,可提高溶解度和通过皮肤传递
Karolina Bilska1, Anna Nowak2, Martyna Zagórska-Dziok2
1West Pomeranian University of Technology in Szczecin, Faculty of Chemical Technology and Engineering, Department of Organic Chemical Technology and Polymer Materials, Piastów Ave. 42, 71-065 Szczecin, Poland; Pomeranian Medical University in Szczecin, Department of Cosmetic and Pharmaceutical Chemistry, Powstańców Wielkopolskich Ave. 72, 70-111 Szczecin, Poland.
概括
一种新的离子合物,L-alaninium borneol ester flurbiprofenate (AlaOBor∙F),显著增强了flurbiprofen的功效.
科学领域:
- 制药化学 制药化学 制药化学
- 药物运输 药物运输 药物运输
- 药用化学 医学化学
背景情况:
- 非类固醇抗炎药物 (NSAID) Flurbiprofen 具有较差的水溶性和有限的皮肤透性.
- 这些局限性阻碍了其在口服和透皮药物输送系统中的生物可用性.
研究的目的:
- 为了合成和描述flurbiprofen的新型离子合物,L-alaninium borneol Ester flurbiprofenate (AlaOBor∙F). 为了合成和描述flurbiprofen的新型离子合物,L-alaninium borneol ester flurbiprofenate (AlaOBor∙F).
- 为了评估与flurbiprofen相比,AlaOBor∙F的增强的物理化学特性和治疗疗效,用于潜在的局部施用.
主要方法:
- 采用了两种合成途径:直接酸催化化和使用二环基二胺的合方法.
- 鉴定包括NMR,FT-IR,DSC,TG和XRD分析.
- 评估了物理化学性质,通过皮的透性 (ex vivo弗朗茨扩散细胞),细胞毒性和抗炎活性.
主要成果:
- 与flurbiprofen相比,AlaOBor∙F显著改善了水溶性和降低了脂性.
- 对AlaOBor∙F.观察到增强的通过皮的透性.
- 结合剂保留了抗氧化活性,没有显著的细胞毒性,并通过减少关键炎症标志物表现出优异的剂量依赖的抗炎作用.
结论:
- 与L-alaninium borneol的离子配对是一种可行的策略,可以克服flurbiprofen的局限性.
- AlaOBor·F 是一个有前途的候选人,可以提高NSAIDs的局部输送和治疗效果.
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